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Assay Detail

CHEMBL1798408

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells by scintillation counting
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, structure-affinity relationships, and molecular modeling studies of novel pyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.
Lenzi O, Colotta V, Catarzi D, Varano F, Squarcialupi L, Filacchioni G, Varani K, Vincenzi F, Borea PA, Dal Ben D, Lambertucci C, Cristalli G.
Bioorg Med Chem (2011) 19 : 3757 -3768
PubMed 21616671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.57 7.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL241987 1 7.51
CHEMBL1795502 1 6.30
CHEMBL320805 1 6.26
CHEMBL1795500 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL241987 Ki = 30.8 nM 7.51
CHEMBL1795502 Ki = 500.0 nM 6.30
CHEMBL320805 Ki = 551.0 nM 6.26
CHEMBL1795500 Ki = 600.0 nM 6.22